Day: November 2, 2022

On November 4, 2021, Xu, Qing; Li, Zhe; Nilar, Shahul published a patent.Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine The title of the patent was Preparation of thienopyrimidines as ferroportin inhibitors. And the patent contained the following:

The invention is related to the preparation of compounds I [R1, R2 = independently H, alkyl, halo, 5- or 6-membered heteroaryl; Z = N, CH; R6 = independently at each occurrence halogen, hydroxy, alkoxy, cycloalkyl, etc.; n = 0-3; Y1 = absent or present; Y1, if present, and Y2, and Y3 = independently selected N, CH, and C (when R6 is attached thereto); R3 = H, alkyl, hydroxyalkyl; R4 = CR4cR4dCONR4aR4b, CH2CH2NR4eR4f, CH2CH2OR4g; R4a = H, alkyl; R4b = H, alkyl, cycloalkyl, 5- to 7-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl; or NR4aR4b = 5- to 7-membered heterocyclyl; R4c i= H, alkyl, cycloalkyl, hydroxyalkyl; R4d = H, alkyl; or CR4cR4d = cycloalkyl or 5- to 7-membered heterocyclyl; R4e = H, alkyl, C5-C10 cycloalkyl, 5- to 7-membered heterocyclyl, and C6-C10 aryl; R4f = H, alkyl; NR4eR4f = 5- to 7-membered heterocyclyl; R4g = H, alkyl, cycloalkyl, 5- to 7-membered heterocyclyl, C6-C10 aryl, and 5- to 10-membered heteroaryl; wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl of R4b, R4c, R4e, and R4g is optionally substituted with 1-2 substituents; with th e exclusion of a specified compound], and pharmaceutical acceptable salts thereof. Pharmaceutical compositions comprising compounds I, and methods of administering compounds I for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries. Thus, II was prepared from 2,4-dichlorothieno[2,3-d]pyrimidine and Et 2-(methylamino)acetate hydrochloride using 4-methoxy-2-(tributylstannyl)pyridine and 5-amino-2-methoxypyridine.. II was tested in an in vitro ferroportin internalization assay (pEC50 = 6.6). The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

The Article related to thienopyrimidine preparation ferroportin inhibitor, preparation thienopyrimidine amino acid amide ferroportin inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 14, 1998, Murugesan, Natesan; Barrish, Joel C.; Stein, Philip D. published a patent.Electric Literature of 160377-42-4 The title of the patent was Preparation of substituted biphenyl sulfonamides as endothelin antagonists. And the patent contained the following:

The title compounds [I; X, Y = N, O; R1, R2 = H, alkyl, alkoxy, OH, etc.; R3, R4 = H, alkyl, alkenyl, alkynyl, alkoxy, etc.; R5 = alkyl, alkenyl, alkynyl, etc.; R11-R14 = H, alkyl, alkenyl, alkoxy, etc.; J, K, T, U = N, C; p = 0-2] are prepared I are useful as endothelin antagonists for the treatment of endothelin-related disorders, hypertension, ischemia, atherosclerosis and related diseases (no data). Thus, N-(3,4-dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4′-(2-pyrimidinyl)-(1,1′-biphenyl)-2-sulfonamide (preparation given) was treated with aqueous HCl to provide 87% the title compound (II). The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).Electric Literature of 160377-42-4

The Article related to sulfonamide biphenyl preparation endothelin antagonist, disorder hypertension ischemia atherosclerosis treatment sulfonamide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 160377-42-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kataev, V. A.; Meshcheryakova, S. A.; Lazarev, V. V.; Kuznetsov, V. V. published an article in 2013, the title of the article was Synthesis of thietanyl-substituted pyrimidine-2,4(1H,3H)-dions.Recommanded Product: 626-48-2 And the article contains the following content:

Reactions of 6-methylpyrimidine-2,4(1H,3H)-dione or 5-hydroxy-6-methyl-pyrimidine-2,4(1H,3H)-dione with 2-chloromethylthiirane afforded the corresponding substituted 1-(thietan-3-yl)pyrimidine-2,4(1H,3H)-diones I, II. The calculations in the framework of approximations PBE/3z, B3LYP/6-31G++(d,p) and MP2/6-31G++(d,p) showed that the alkylation occurred at the atom N1 of the pyrimidine ring. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Recommanded Product: 626-48-2

The Article related to thietanylpyrimidinedione preparation, methylpyrimidinedione hydroxymethylpyrimidinedione chloromethylthiirane free gibbs energy, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 31, 2021, Kataev, V. A.; Mesheryakova, S. A.; Mesheryakova, E. S.; Tyumkina, T. V.; Khalilov, L. M.; Lazarev, V. V.; Kuznetsov, V. V. published an article.Computed Properties of 626-48-2 The title of the article was Synthesis, Structure, and Conformational Analysis of N-(2,4-Dichlorophenyl)-2-[6-methyl-2,4-dioxo-3-(thietan-3-yl)-1,2,3,4-tetrahydropyrimidine-1-yl]acetamide. And the article contained the following:

The reaction of 6-methyluracil with 2-chloromethyltiiran afforded 6-methyl-3-(thietan-3-yl)uracil. Its subsequent reaction with N-(2,6-dichlorophenyl)-2-chloroacetamide resulted in N-(2,4-dichlorophenyl)-2-[6-methyl-2,4-dioxo-3-(thietan-3-yl)-1,2,3,4-tetrahydropyrimidin-1-yl]acetamide, proved by X-ray anal., NMR and IR spectroscopy. Computer modeling at the PBE/3ζ, PBE/cc-pVDZ and PBE/SV(P) levels showed that its conformational behavior is determined by internal rotation of the thietanyl group both in the gas phase and in chloroform or DMSO solutions The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Computed Properties of 626-48-2

The Article related to dichlorophenyl methyl dioxothietanyltetrahydropyrimidinyl acetamide preparation crystal structure conformational transformation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Jakubkiene, Virginija; Valiulis, Gabrielius Ernis; Schweipert, Markus; Zubriene, Asta; Matulis, Daumantas; Meyer-Almes, Franz-Josef; Tumkevicius, Sigitas published an article in 2022, the title of the article was Synthesis and HDAC inhibitory activity of pyrimidine-based hydroxamic acids.COA of Formula: C5H6N2O2 And the article contains the following content:

Here, the synthesis of new compounds in which a hydroxamic acid residue was attached to differently substituted pyrimidine rings via a methylene group bridge of varying length as potential HDAC inhibitors was described. The target compounds were obtained by alkylation of 2-(alkylthio)pyrimidin-4(3H)-ones with Et 2-bromoethanoate, Et 4-bromobutanoate, or Me 6-bromohexanoate followed by aminolysis of the obtained esters with hydroxylamine. Oxidation of the 2-methylthio group to the methylsulfonyl group and following treatment with amines resulted in the formation of the corresponding 2-amino-substituted derivatives, the ester group of which reacted with hydroxylamine to give the corresponding hydroxamic acids. The synthesized hydroxamic acids were tested as inhibitors of the HDAC4 and HDAC8 isoforms. Among the synthesized pyrimidine-based hydroxamic acids -hydroxy-6-[6-methyl-2-(methylthio)-5-propylpyrimidin-4-yloxy]hexanamide was found to be the most potent inhibitor of both the HDAC4 and HDAC8 isoforms, with an IC50 of 16.6μM and 1.2μM, resp. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).COA of Formula: C5H6N2O2

The Article related to pyrimidine based hydroxamic acid preparation hdac inhibitor, hdac inhibitors, alkylation, aminolysis, hydroxamic acid, pyrimidine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C5H6N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 12, 2012, Nakamura, Tsuyoshi; Namiki, Hidenori; Terasaka, Naoki; Shima, Akiko; Hagihara, Masahiko; Iwase, Noriaki; Takata, Katsunori; Kikuchi, Osamu; Tsuboike, Kazunari; Setoguchi, Hiroyuki; Yoneda, Kenji; Sunamoto, Hidetoshi; Ito, Koji published a patent.Formula: C7H9ClN2 The title of the patent was Preparation of tetrahydroquinoline compounds as CETP inhibitors. And the patent contained the following:

Title compounds I [R1 = H, alkyl, hydroxyalkyl, etc.; or pharmacol. acceptable salts thereof], useful for the treatment of dyslipidemia, hypercholesterolemia, arteriosclerosis, etc., were prepared For example, conversion of 4,4-difluorocyclohexanecarboxylic acid Et ester into II [PMB = p-methoxybenzyl] in a multi-step process followed by treatment with 4-CF3PhMgBr, diastereomeric separation, fluorination, de-alkoxycarbonylation, chiral separation, reaction with 2-bromopyrimidine, and debenzylation afforded compound III [R = pyrimidin-2-yl]. In CETP (cholesteryl ester transfer protein) inhibition assays, IC50 of III [R = 5-(4-methylpiperazin-1-yl)pyrimdin-2-yl] was 19 nM. Pharmaceutical formulations containing I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Formula: C7H9ClN2

The Article related to tetrahydroquinoline preparation cetp inhibitor, dyslipidemia hypercholesterolemia arteriosclerosis treatment tetrahydroquinoline cetp inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C7H9ClN2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 4, 1985, Boehm, Ralf; Haubold, Gudrun; Pech, Reinhard; Laban, Gunter published a patent.Quality Control of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine The title of the patent was Arylamino-substituted thieno[2,3-d]pyrimidines. And the patent contained the following:

Blood platelet aggregation inhibiting (no data) title compounds [I; R1 = R2 = Me; R1R2 = (CH2)4; R3 = R5 = H; R4 = R6 = aryl; R5R6N = saturated, monocyclic heterocydyl] were prepared by aminolysis of 2,4-dichlorothieno[2,3-d]pyrimidines. Thus, 2,4-dichloro-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine was refluxed 6 h with 2-MeC6H4NH2 in PrOH to give 2-o-toluidino derivative II (R7 = Cl). This was refluxed with morpholine to give II (R7 = morpholino). The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Quality Control of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

The Article related to blood platelet aggregation inhibition thienopyrimidinediamine, thienopyrimidinediamine, benzothienopyrimidinediamine, aminolysis chlorothienopyrimidine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Slyvka, Natalia; Gevaza, Yuri; Saliyeva, Lesya published an article in 2018, the title of the article was Electrophilic Intramolecular Cyclization of 1-(N-alkenyl)-6-methylpyrimidine-2,4-diones.Recommanded Product: 626-48-2 And the article contains the following content:

N-allyl(cinnamyl)substituted derivatives of 6-methyluracil I (R = H, C6H5) were synthesized. The reactions of their bromo- and iodocyclization were performed which led to the formation of the derivatives of dihydrooxazolopyrimidinium II·X (R1 = Br, I; X = Br3-, I3-) and dihydrooxazinepyrimidinium III·X (R1 = Br, I; X = Br3-, I3-; R2 = H, cinnamyl). The factors that favor the regioselectivity of these reactions were suggested. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Recommanded Product: 626-48-2

The Article related to oxazolopyrimidinium salt preparation regioselective, methyl pyrimidine dione alkenyl halocyclization, oxazinepyrimidinium salt preparation regioselective, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 4, 2022, Li, Jian; Li, Jiaming; He, Runfa; Liu, Jiasheng; Liu, Yang; Chen, Lu; Huang, Yubing; Li, Yibiao published an article.Related Products of 160377-42-4 The title of the article was Selective Synthesis of Substituted Pyridines and Pyrimidines through Cascade Annulation of Isopropene Derivatives. And the article contained the following:

Diverse substituted pyridines I (R = H, Me; R1 = n-Bu, thiophen-2-yl, 4-chlorophenyl, etc.) and pyrimidines II with high selectivity were obtained using a concise and efficient protocol. The reaction proceeds via metal-free cascade annulation of isopropene derivatives R1C(=CH2)CH2R. Using isopropene derivatives as C3 synthons, NH4I as the “N” source, and formaldehyde or DMSO as the carbon source, this reaction realizes the efficient formation of intermol. C-N and C-C bonds. The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).Related Products of 160377-42-4

The Article related to methylpyridine preparation, pyrimidine preparation, isopropene formaldehyde tandem heterocyclization, dimethyl sulfoxide isopropene tandem heterocyclization, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 160377-42-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On November 1, 2013, Lukmanov, Timur; Ivanov, Sergey P.; Khamitov, Edward M.; Khursan, Sergey L. published an article.SDS of cas: 626-48-2 The title of the article was Relative stability of keto-enol tautomers in 5,6-substituted uracils: Ab initio, DFT and PCM study. And the article contained the following:

The relative stability orders in the tautomers of uracil and its derivatives (5-fluorouracil, 5-chlorouracil, 5-aminouracil, 5-hydroxyuracil, 5-methyluracil, 6-methyluracil, 5-hydroxy-6-methyluracil and 5-amino-6-methyluracil) were established using composite (G3MP2B3) and DFT (TPSS) methods. The stability orders were determined both in the gas phase and water solutions, taking into account specific and non-specific hydration. The primary solvation shell of uracils was modeled as a complex of a tautomer with 5 water mols. An anal. of the factors which determine the stability of the enol forms of uracils was performed. The most important factor was found to be changes in the intramol. conjugation at tautomerization. As was shown by the NBO anal., the stabilization energy due to the nN → π* (or σ*) interaction in the diketo tautomer is lost in the enol forms, but is partially compensated by an increase in the conjugation length. The effect of the substituent in the fifth position of the pyrimidine ring on the energy of tautomers is less prominent. It was shown that the hydration energy considerably differs for tautomers, and leads to substantial redistribution in the stability series of uracil tautomers. Both specific and non-specific solvation are of vital importance for stabilization of tautomers. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).SDS of cas: 626-48-2

The Article related to uracil keto enol tautomer relative stability, Physical Organic Chemistry: Acid-Base, Tautomerism, and Other Equilibrium Studies and other aspects.SDS of cas: 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia